PNU-74654 inhibits the Wnt-β catenin pathway by blocking the interaction between β-catenin and TCF (T cell factor). PNU-74654 is also an anti-tumor agent. Aberrant activation of the Wnt/β-catenin pathway (canonical pathway) is implicated in driving development/progression of different tumors, such as colon cancer, through interaction between β-catenin and T cell factor (TCF), which regulates the expression of target genes in cell proliferation and differentiation. Inhibition of this pathway activity in cancer cell lines efficiently blocks their growth. PNU-74654 inhibits this pathway by blocking the interaction between β-catenin and TCF.
| Molecular Weight | 320.34 |
| Formula | C19H16N2O3 |
| CAS Number | 113906-27-7 |
| Solubility (25°C) | DMSO: ≥10 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Related Wnt/beta-catenin Products |
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| FZD7 antagonist 1
FZD7 antagonist 1 (peptide 34) is a dFz7-21 analogue. |
| NLS-StAx-h
NLS-StAx-h is a selective, cell permeable, stapled peptide Wnt signaling inhibitor with an IC50 of 1.4 μM. |
| Zamaporvint
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| Foxy-5
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